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1. 发明申请

WO2005055980A3 POLYMALIC ACID-BASED MULTIFUNCTIONAL DRUG DELIVERY SYSTEM 审中-公开
标题翻译：基于聚合酸的多功能药物递送系统
公开(公告)号：WO2005055980A3
公开(公告)日：2006-01-05
申请号：PCT/US2004040660
申请日：2004-12-03
申请人： ARROGENE INC , LJUBIMOVA JULIA Y , BLACK KEITH L , HOLLER EGGEHARD
发明人： LJUBIMOVA JULIA Y , BLACK KEITH L , HOLLER EGGEHARD
IPC分类号： A61K47/48
CPC分类号： A61K47/6883 , A61K47/593 , A61K47/60
摘要： A structured drug system that is useful for delivering a drug payload to a specific tissue or cell type is disclosed. The system is based on purified polymalic acid. This polymer isolated from natural sources is biocompatible, biodegradable and of very low toxicity. The polymer is extremely water soluble and contains a large number of free carboxyl groups which can used to attach a number of different active molecules. In the examples disclosed N-hydroxysuccinimide esters of the carboxyl groups are used to attach such molecules. The active molecules include monoclonal antibodies to promote specific cellular uptake and specific pro-drugs such as antisense nucleic acids designed to modify the cellular metabolism of a target cell. The pro-drugs are advantageously linked by a somewhat labile bond so that they will be released under specific conditions. In addition, the system contains amide-linked valine to encourage membrane disruption under lysosomal conditions. Polyethylene glycol groups are attached to extend the drug system's circulation half-life. In addition, fluorescent reported groups can be readily included to aid in visualizing and confirming drug system targeting. The drug system can deliver treatments for a wide range of diseases and is specially advantageous for treatment of neoplasms.
摘要翻译：公开了一种用于将药物有效载荷递送到特定组织或细胞类型的结构化药物系统。该系统基于纯化的聚丙酸。从天然来源分离的聚合物是生物相容的，可生物降解的和非常低的毒性。聚合物极易水溶，并含有大量游离羧基，可用于连接许多不同的活性分子。在实施例中，羧基的N-羟基琥珀酰亚胺酯用于附着这些分子。活性分子包括促进特异性细胞摄取的单克隆抗体和特异性前体药物，例如旨在修饰靶细胞的细胞代谢的反义核酸。前药有利地通过稍微不稳定的键连接，使得它们将在特定条件下释放。此外，该系统含有酰胺键缬氨酸，以促进溶酶体条件下的膜破坏。连接聚乙二醇基团以延长药物系统的循环半衰期。此外，可以容易地包括荧光报告的组以帮助可视化和确认药物系统靶向。药物系统可以为广泛的疾病提供治疗，特别有利于治疗肿瘤。

2. 发明专利

IL261438D0 Polymalic acid based nanoimmunoconjugates and uses thereof 未知
公开(公告)号：IL261438D0
公开(公告)日：2018-10-31
申请号：IL26143818
申请日：2018-08-28
申请人： CEDARS SINAI MEDICAL CENTER , LJUBIMOVA JULIA Y , BLACK KEITH L , HOLLER EGGEHARD , LJUBIMOV ALEXANDER , DING HUI
发明人： LJUBIMOVA JULIA Y , BLACK KEITH L , HOLLER EGGEHARD , LJUBIMOV ALEXANDER , DING HUI
IPC分类号： A61K20060101
摘要： Nanoimmunoconjugates including a polymalic acid-based molecular scaffold, targeting ligands, anti-tumor immune response stimulators and anti-cancer agents are provided. Methods for treating cancer in a subject by administering the nanoimmunoconjugates that provide both systemic and local immune responses and synergistic anticancer effect are described.

3. 发明专利

JP2010163468A Polymalic acid-based multifunctional drug delivery system 审中-公开
标题翻译：基于聚合酸的多功能药物递送系统
公开(公告)号：JP2010163468A
公开(公告)日：2010-07-29
申请号：JP2010107780
申请日：2010-05-07
申请人： Arrogene Inc , Cedars-Sinai Medical Center , アロジーン, インコーポレイテッド , セダーズ−シナイメディカルセンター
发明人： LJUBIMOVA JULIA Y , BLACK KEITH L , HOLLER EGGEHARD
IPC分类号： A61K47/42 , A61K31/711 , A61K47/34 , A61K47/48 , A61P35/00 , A61P43/00
CPC分类号： A61K47/6883 , A61K47/593 , A61K47/60
摘要： PROBLEM TO BE SOLVED: To provide a structured drug system that is useful for delivering a drug payload to a specific tissue or cell type. SOLUTION: The system is based on purified polymalic acid. This polymer isolated from natural sources is biocompatible, biodegradable and of very low toxicity. The polymer is extremely water soluble and contains a large number of free carboxyl groups which can be used to attach a number of different active molecules. In the examples disclosed N-hydroxysuccinimide esters of the carboxyl groups are used to attach such molecules. The active molecules include monoclonal antibodies to promote specific cellular uptake and specific pro-drugs such as antisense nucleic acids designed to modify the cellular metabolism of a target cell. The pro-drugs are advantageously linked by a somewhat labile bond so that they will be released under specific conditions. COPYRIGHT: (C)2010,JPO&INPIT
摘要翻译：要解决的问题：提供可用于将药物有效载荷递送到特定组织或细胞类型的结构化药物系统。解决方案：该系统基于纯化的聚丙酸。从天然来源分离的聚合物是生物相容的，可生物降解的，毒性非常低。该聚合物极易溶于水并含有大量游离羧基，可用于连接许多不同的活性分子。在实施例中，羧基的N-羟基琥珀酰亚胺酯用于附着这些分子。活性分子包括促进特异性细胞摄取的单克隆抗体和特异性前体药物，例如旨在修饰靶细胞的细胞代谢的反义核酸。前药有利地通过稍微不稳定的键连接，使得它们将在特定条件下释放。版权所有（C）2010，JPO＆INPIT

4. 发明专利

ES2717836T3 Sistema de administración de fármacos multifuncional a base de ácido polimálico 未知
公开(公告)号：ES2717836T3
公开(公告)日：2019-06-25
申请号：ES04813049
申请日：2004-12-03
申请人： ARROGENE INC , CEDARS SINAI MEDICAL CENTER
发明人： LJUBIMOVA JULIA , BLACK KEITH , HOLLER EGGEHARD
IPC分类号： A61K47/59 , A61K47/48 , A61K47/60 , A61K47/68 , A61P35/00

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